This invention relates to the use of norgestrel, its D- and L-enantiomers and their 17-esters as neuropsychotropic agents and to compositions comprising the L-enantiomer.
Norgestrel (DL-13-ethyl-17.alpha.-ethynyl-17.beta.-hydroxy-4-gonen-3-one), its D- and L-enantiomers and their 17-esters are known. See for example, German Pat. Nos. 1,468,604 and 1,493,161.
Several steroids are known to exert depressant effect on the central nervous system and have hypnotic and/or anesthetic effects. These steroids are not useful in accordance with this invention, due to their known side effects, for example, an undesired depression of the central nervous system.
Minor tranquilizers of the benzodiazepine type have become popular as medicinal agents having anxiolytic and sedative activity. However, these active agents have the disadvantage that their use can cause a psychic dependency (WHO Bull. 43 Suppl., 1970: 49). Upon prolonged usage, there is also the danger of tolerance development. Furthermore, the muscle-relaxant properties of these compounds can lead to undesirable side effects (AMA Drug Evaluations, American Medical Assoc. Chicago, 1st ed. [1971]: N 47 et seq.).
Tricyclic neuroleptics are generally known, such as, for example, phenothiazine and the butyrophenones, as medicinal agents having a neuroleptic effect. These compounds result, even in normal doses, in extrapyramidal side effects. As a later consequence, tardive dyskinesia can occur.
It has now been found that norgestrel, its enantiomers and their 17-esters, exhibit a spectrum of activity which is broader than the conventional tranquilizers; more particularly, they possess neuropsychotropic activity of the major tranquilizer type, especially sedative and neuroleptic activity, with the additional advantage that they do not possess the aforementioned side effects.
For examples of other steroids having a broader spectrum of effectiveness, compared to conventional minor tranquilizers, see U.S. Pat. Nos. 3,895,110 and 3,908,007.